Details
| Original language | English |
|---|---|
| Pages (from-to) | 1681-1689 |
| Number of pages | 9 |
| Journal | MEDCHEMCOMM |
| Volume | 8 |
| Issue number | 8 |
| Publication status | Published - Jun 2017 |
| Externally published | Yes |
Abstract
A series of gold(i) complexes with two N-heterocyclic carbene ligands (biscarbene gold complexes) were prepared and evaluated for their effects against cancer cells and pathogenic bacteria. Proliferation inhibition was observed in cancer cells and in Gram-positive bacteria, whereas Gram-negative bacteria were less sensitive towards the compounds. The protein binding and cellular uptake were quantified and the combined results indicated a strong correlation between cellular bioavailability and antiproliferative effects. The biscarbene gold complexes inhibited bacterial and mammalian TrxRs with low to moderate potency. However, based on the obtained structure-activity-relationships and the high cellular accumulation levels, TrxR inhibition can be considered as a relevant contributor to the cellular pharmacology of biscarbene gold(i) complexes.
ASJC Scopus subject areas
- Biochemistry, Genetics and Molecular Biology(all)
- Biochemistry
- Biochemistry, Genetics and Molecular Biology(all)
- Molecular Medicine
- Pharmacology, Toxicology and Pharmaceutics(all)
- Pharmacology
- Pharmacology, Toxicology and Pharmaceutics(all)
- Pharmaceutical Science
- Pharmacology, Toxicology and Pharmaceutics(all)
- Drug Discovery
- Chemistry(all)
- Organic Chemistry
Sustainable Development Goals
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In: MEDCHEMCOMM, Vol. 8, No. 8, 06.2017, p. 1681-1689.
Research output: Contribution to journal › Article › Research › peer review
}
TY - JOUR
T1 - Biscarbene gold(i) complexes
T2 - Structure-activity-relationships regarding antibacterial effects, cytotoxicity, TrxR inhibition and cellular bioavailability
AU - Schmidt, Claudia
AU - Karge, Bianka
AU - Misgeld, Rainer
AU - Prokop, Aram
AU - Brönstrup, Mark
AU - Ott, Ingo
N1 - Funding Information: Financial support from Deutsche Forschungsgemeinschaft (DFG) is gratefully acknowledged (project codes: OT338/12-1 and BR3572/4-1). We thank Dr. Raimo Franke (HZI) for fruitful discussions and his support of this study.
PY - 2017/6
Y1 - 2017/6
N2 - A series of gold(i) complexes with two N-heterocyclic carbene ligands (biscarbene gold complexes) were prepared and evaluated for their effects against cancer cells and pathogenic bacteria. Proliferation inhibition was observed in cancer cells and in Gram-positive bacteria, whereas Gram-negative bacteria were less sensitive towards the compounds. The protein binding and cellular uptake were quantified and the combined results indicated a strong correlation between cellular bioavailability and antiproliferative effects. The biscarbene gold complexes inhibited bacterial and mammalian TrxRs with low to moderate potency. However, based on the obtained structure-activity-relationships and the high cellular accumulation levels, TrxR inhibition can be considered as a relevant contributor to the cellular pharmacology of biscarbene gold(i) complexes.
AB - A series of gold(i) complexes with two N-heterocyclic carbene ligands (biscarbene gold complexes) were prepared and evaluated for their effects against cancer cells and pathogenic bacteria. Proliferation inhibition was observed in cancer cells and in Gram-positive bacteria, whereas Gram-negative bacteria were less sensitive towards the compounds. The protein binding and cellular uptake were quantified and the combined results indicated a strong correlation between cellular bioavailability and antiproliferative effects. The biscarbene gold complexes inhibited bacterial and mammalian TrxRs with low to moderate potency. However, based on the obtained structure-activity-relationships and the high cellular accumulation levels, TrxR inhibition can be considered as a relevant contributor to the cellular pharmacology of biscarbene gold(i) complexes.
UR - http://www.scopus.com/inward/record.url?scp=85027526082&partnerID=8YFLogxK
U2 - 10.1039/c7md00269f
DO - 10.1039/c7md00269f
M3 - Article
AN - SCOPUS:85027526082
VL - 8
SP - 1681
EP - 1689
JO - MEDCHEMCOMM
JF - MEDCHEMCOMM
SN - 2040-2503
IS - 8
ER -